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RWJ-56110 dihydrochloride Sale

目录号 : GC61777

RWJ-56110dihydrochloride是一种有效的、选择性的、拟肽抑制剂,抑制PAR-1激活和内化(结合IC50=0.44uM),对PAR-2,PAR-3和PAR-4无影响。RWJ-56110dihydrochloride抑制由SFLLRN-NH2 (IC50=0.16μM)和凝血酶(IC50=0.34μM)诱导的血小板聚集,相对于U46619具有相当的选择性。RWJ-56110dihydrochloride在体内阻断血管生成和新血管的形成。RWJ-56110dihydrochloride诱导细胞凋亡(apoptosis)。

RWJ-56110 dihydrochloride Chemical Structure

Cas No.:2387505-58-8

规格 价格 库存 购买数量
5 mg
¥5,220.00
现货
10 mg
¥8,820.00
现货
25 mg
¥17,100.00
现货
50 mg
¥28,800.00
现货
100 mg
¥45,000.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis[1][2].

Proteinase-activated receptors (PARs) are a family of G protein-coupled receptors activated by the proteolytic cleavage of their N-terminal extracellular domain, exposing a new amino terminal sequence that functions as a tethered ligand to activate the receptors.RWJ56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM) while being quite selective relative to collagen and the thromboxane mimetic U46619 [1].RWJ-56110 dihydrochloride is fully inhibits thrombin-induced RASMC proliferation with an IC50 value of 3.5 μM. RWJ-56110 dihydrochloride shows blockade of thrombin's action with RASMC calcium mobilization (IC50=0.12 μM), as well as with HMVEC (IC50=0.13 μM) and HASMC calcium mobilization (IC50=0.17 μM)[1].RWJ56110 (0.1-10 μM; 24-96 hours) inhibits endothelial cell growth dose-dependently, with half-maximal inhibitory concentration of RWJ56110 is approximately 10 μM[2].RWJ56110 (0.1-10 μM; 6 hours) inhibits DNA synthesis of endothelial cells in a thymidine incorporation assays. Endothelial cells are in fast-growing state (50-60% confluence), RWJ56110 inhibits cell DNA synthesis in a dose-dependent manner, but when cells that are in the quiescent state (100% confluent), the inhibitory effect of PAR-1 antagonists is much less pronounced[2].RWJ56110 (0.1-10 μM; pretreatment for 15 min) inhibits thrombin-induced Erk1/2 activation in a concentration-dependent manner. However, when endothelial cells are stimulated by FBS (final concentration 4%), it reduces partially the activated levels of Erk1/2[2].RWJ56110 (30 μM; 24 hours) has an inhibitory effect on endothelial cell cycle progression. It reduces the percentage of cells in the S phase, while alterations in the percentages of G1 and G2/M cells are less pronounced[2]. Western Blot Analysis[2] Cell Line: Endothelial cells

[1]. Andrade-Gordon, et al.Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. oc Natl Acad Sci U S A. 1999 Oct 26;96(22):12257-62. [2]. Panagiota Zania, et al. Blockade of angiogenesis by small molecule antagonists to protease-activated receptor-1: association with endothelial cell growth suppression and induction of apoptosis. J Pharmacol Exp Ther. 2006 Jul;318(1):246-54.

Chemical Properties

Cas No. 2387505-58-8 SDF
Canonical SMILES O=C(N[C@H](C(NCC1=CC=CC=C1)=O)CCN)[C@@H](NC(NC2=CC3=C(C=C2)C(CN4CCCC4)=CN3CC5=C(Cl)C=CC=C5Cl)=O)CC6=CC=C(F)C(F)=C6.[H]Cl.[H]Cl
分子式 C41H45Cl4F2N7O3 分子量 863.65
溶解度 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 1.1579 mL 5.7894 mL 11.5788 mL
5 mM 0.2316 mL 1.1579 mL 2.3158 mL
10 mM 0.1158 mL 0.5789 mL 1.1579 mL
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